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Literature summary for 3.4.23.39 extracted from

  • Dahlgren, A.; Kvarnstrom, I.; Vrang, L.; Hamelink, E.; Hallberg, A.; Rosenquist, A.; Samuelsson, B.
    New inhibitors of the malaria aspartyl proteases plasmepsin I and II (2003), Bioorg. Med. Chem., 11, 3423-3437.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-((1S,2R)-2-hydroxyindan-1-yl)-butyramide 0.005 mM, 25% inhibition Plasmodium falciparum
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide 0.005 mM, 68% inhibition Plasmodium falciparum
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-ylethyl)-butyramide 0.005 mM, 74% inhibition Plasmodium falciparum
(2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide 0.005 mM, 39% of maximal activity Plasmodium falciparum
(2R,3R)-4-(N-benzyloxycarbonylbenzylamino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide 0.005 mM, 40% inhibition Plasmodium falciparum
(2R,3R)-4-(N-benzyloxycarbonylbenzylamino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide 0.005 mM, 54% inhibition Plasmodium falciparum
(2R,3R)-4-[((S)-2-N-benzyloxycarbonylamino-3-methylbutyryl)-benzylamino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide 0.005 mM, 43% inhibition Plasmodium falciparum
(2R,3R)-4-[((S)-2-N-benzyloxycarbonylamino-3-methylbutyryl)-benzylamino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide 0.005 mM, 64% inhibition Plasmodium falciparum
(2R,3R)-4-[N-benzyl-N'-((S)-2-benzyloxycarbonylamino-3-methyl-butyryl)-hydrazino]-2-(4-bromobenzyloxy)-3-hydroxy-N-(pyridin-3-yl-methyl)-butyramide 0.005 mM, 50% inhibition Plasmodium falciparum
(2R,3R)-4-[N-benzyl-N'-((S)-2-tert-butyloxycarbonyl-amino-3-methyl-butyryl)-hydrazino]-2-(4-bromobenzyloxy)-3-hydroxy-N-((1S,2R)-2-hydroxy-indan-1-yl)-butyramide 0.005 mM, 49% inhibition Plasmodium falciparum
(2S,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide 0.005 mM, 35% inhibition Plasmodium falciparum
(2S,3S)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide 0.005 mM, 20% inhibition Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0014
-
 (2R,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-ylethyl)-butyramide
-
 Plasmodium falciparum
0.003
-
 (2S,3R)-4-(N-benzyl-N'-benzyloxycarbonyl-hydrazino)-2-(4-bromobenzyloxy)-3-hydroxy-N-(2-piperidin-1-yl-ethyl)-butyramide
-
 Plasmodium falciparum